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Ester derivatives and medicinal use thereof

An ester compound, C1-C6 technology, applied in pharmaceutical formulations, medical preparations containing active ingredients, drug combinations, etc.

Inactive Publication Date: 2007-10-17
JAPAN TOBACCO INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, in this patent, there is no disclosure or suggestion of data showing that the disclosed compound selectively inhibits MTP in the small intestine with little effect on MTP in the liver

Method used

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  • Ester derivatives and medicinal use thereof
  • Ester derivatives and medicinal use thereof
  • Ester derivatives and medicinal use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0700] The present invention is explained in detail by the following examples, reference examples, test examples, and preparation examples, but it goes without saying that the present invention is limited thereto.

reference example 1

[0702] Preparation of 6-methyl-2-(4-trifluoromethylphenyl)nicotinic acid

[0703]

[0704] In the above reaction scheme, Me is methyl, WSC is 1-ethyl-3-(3'-dimethylaminopropyl) carbodiimide, DMAP is dimethylaminopyridine, and DMF is dimethyl formazan amides. Hereinafter, each symbol is the same as defined above.

[0705] a) Methyl 2-chloro-6-methylnicotinate

[0706] 2-Chloro-6-methylnicotinic acid (25.0 g) was suspended in a mixed solvent of dimethylformamide (100 mL) and chloroform (100 mL), and dimethylaminopyridine (21.3 g) and Methanol (4.67 g), and finally, 1-ethyl-3-(3'-dimethylaminopropyl) carbodiimide (WSC) hydrochloride (33.5 g) was added to the mixture, which was then stirred at room temperature After 6 hours, the reaction mixture was concentrated, ethyl acetate (300 mL) was added thereto, the mixture was washed successively with water, 10% ammonium chloride, water, and saturated brine, dried over sodium sulfate, and concentrated, and the residue was subjected...

reference example 2

[0713] Preparation of 3-ethyl-5-fluoro-4-hydroxybenzoic acid methyl ester

[0714]

[0715] In the above reaction scheme, Me is a methyl group; conc.H 2 SO 4 is concentrated sulfuric acid; NBS is N-bromosuccinimide; THF is tetrahydrofuran; MOMCl is chloromethyl methyl ether; nBu is n-butyl; PdCl 2 (PPh 3 ) 2 is dichlorobis(triphenylphosphine)palladium(II); Pd / C is palladium-carbon, and Et is ethyl. Hereinafter, each symbol is the same as defined above.

[0716]a) Methyl 3-fluoro-4-hydroxybenzoate

[0717] To a solution of 3-fluoro-4-hydroxybenzoic acid (3.0 g) in methanol (30 mL) was added concentrated sulfuric acid (3 mL), the mixture was heated to reflux for 5 hours, the reaction solution was left to cool to room temperature, and then concentrated in vacuo. The residue was diluted with ethyl acetate, washed successively with water, saturated aqueous sodium bicarbonate solution, water, and saturated brine, dried over anhydrous sodium sulfate, and concentrated to give...

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PUM

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Abstract

The invention relates to an ester compound which is indicated by a formula (1) or the medical salt or the usage. The compound of the formula (1) or the medical salt can be used as the treatment agent or the prevention agent of hyperlipidemia etc., thus the ester compound or the medical salt can rapidly disappear in a living body and has excellent MTP inhibition activity.

Description

technical field [0001] The present invention relates to a novel ester derivative, and also to a pharmaceutical composition comprising the novel ester derivative, which selectively inhibits microsomal triglyceride transfer protein (hereinafter also abbreviated as MTP) in the small intestine, or a pharmaceutically acceptable salt thereof . In addition, the present invention relates to therapeutic or preventive agents for hyperlipidemia, arteriosclerosis, coronary artery disease, obesity, diabetes, or hypertension, including novel esters or pharmaceutically acceptable salts thereof that selectively inhibit MTP in the small intestine as an active ingredient. In addition, the present invention relates to a therapeutic or preventive agent for hyperlipidemia, arteriosclerosis, coronary artery disease, obesity, diabetes or hypertension, which has a novel function that has never been known before. Background technique [0002] It is said that hyperlipidemia, diabetes and hypertensi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/24A61K31/277A61K31/40A61K31/4245A61K31/4418A61K31/444A61K31/445A61K31/5375A61K45/00A61P3/04A61P3/06A61P3/10A61P9/10
Inventor 萩原笃池之上拓栗原一典谷口寿生高桥满饭田聪夫
Owner JAPAN TOBACCO INC
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